2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, preparation method thereof, and pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as active ingredient
Dae Yoon Chi,Byoung Se Lee,Youjung Jung,Uthaiwan Sirion,Yoo Jin Lim,Yu Jin Bae,Heejun Kim,So Young Chu,Dae Hyuk Moon,Jin-Sook Ryu,Jae Seung Kim,Seung Jun Oh
申请号:
US12579789
公开号:
US08497260B2
申请日:
2009.10.15
申请国别(地区):
US
年份:
2013
代理人:
摘要:
2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for β-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimers disease at an early stage by non-invasive techniques when they are labeled with radioisotopes:wherein R1-R4, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight β-amyloid peptide binding compound, generation of malignant high-molecular weight β-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimers disease.